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TitleActivation and Signaling Mechanism Revealed by Cannabinoid Receptor-G Complex Structures.
Journal, issue, pagesCell, Vol. 180, Issue 4, Page 655-665.e18, Year 2020
Publish dateFeb 20, 2020
AuthorsTian Hua / Xiaoting Li / Lijie Wu / Christos Iliopoulos-Tsoutsouvas / Yuxia Wang / Meng Wu / Ling Shen / Christina A Brust / Spyros P Nikas / Feng Song / Xiyong Song / Shuguang Yuan / Qianqian Sun / Yiran Wu / Shan Jiang / Travis W Grim / Othman Benchama / Edward L Stahl / Nikolai Zvonok / Suwen Zhao / Laura M Bohn / Alexandros Makriyannis / Zhi-Jie Liu /
PubMed AbstractHuman endocannabinoid systems modulate multiple physiological processes mainly through the activation of cannabinoid receptors CB1 and CB2. Their high sequence similarity, low agonist selectivity, ...Human endocannabinoid systems modulate multiple physiological processes mainly through the activation of cannabinoid receptors CB1 and CB2. Their high sequence similarity, low agonist selectivity, and lack of activation and G protein-coupling knowledge have hindered the development of therapeutic applications. Importantly, missing structural information has significantly held back the development of promising CB2-selective agonist drugs for treating inflammatory and neuropathic pain without the psychoactivity of CB1. Here, we report the cryoelectron microscopy structures of synthetic cannabinoid-bound CB2 and CB1 in complex with G, as well as agonist-bound CB2 crystal structure. Of important scientific and therapeutic benefit, our results reveal a diverse activation and signaling mechanism, the structural basis of CB2-selective agonists design, and the unexpected interaction of cholesterol with CB1, suggestive of its endogenous allosteric modulating role.
External linksCell / PubMed:32004463 / PubMed Central
MethodsEM (single particle) / X-ray diffraction
Resolution2.9 - 3.2 Å
Structure data

EMDB-0744, PDB-6kpf:
Cryo-EM structure of a class A GPCR with G protein complex
Method: EM (single particle) / Resolution: 2.9 Å

EMDB-0745, PDB-6kpg:
Cryo-EM structure of CB1-G protein complex
Method: EM (single particle) / Resolution: 3.0 Å

PDB-6kpc:
Crystal structure of an agonist bound GPCR
Method: X-RAY DIFFRACTION / Resolution: 3.2 Å

Chemicals

ChemComp-E3R:
7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]- 7-methyloctanenitrile

ChemComp-8D0:
(6~{a}~{R},9~{R},10~{a}~{R})-9-(hydroxymethyl)-3-(8-isothiocyanato-2-methyl-octan-2-yl)-6,6-dimethyl-6~{a},7,8,9,10,10~{a}-hexahydrobenzo[c]chromen-1-ol

Source
  • homo sapiens (human)
  • enterobacteria phage rb59 (virus)
KeywordsMEMBRANE PROTEIN / GPCR / LCP / agonist / Gi Protein / G protein / cryo-EM

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